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以二茂铁为起始原料,首先用合成的乙酰基二茂铁与醛反应,合成1-二茂铁基-3-(4-R1苯基)-2-丙烯酮,然后再与水合肼反应合成吡唑啉,最后通过与酰氯反应生成一系列N-酰基-3-二茂铁基-5-芳基吡唑啉化合物。通过1HNMR、FTIR及ESI-HRMS进行了目标化合物结构的表征;最后,将合成的吡唑啉化合物分别对4种植物真菌病(小麦赤霉病、马铃薯干腐病、烟草赤星病、西瓜枯萎病)进行了初步的抗植物真菌活性实验,测试结果显示,部分化合物具有良好的抗植物真菌活性。 相似文献
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以苄氧乙酸和异硫氰酸苯酯为原料,经肼解、环化制得中间体3-氯甲基-5-环戊硫基-4-苯基-4H-1,2,4-三唑后,再与对位卤素取代苯酚反应得到4个新型的标题化合物。其结构经红外、质谱、核磁共振氢谱及元素分析确认。初步生物活性研究结果表明,在实验浓度下该系列化合物表现出一定的杀菌活性。 相似文献
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以二茂铁为原料,首先与乙酸酐发生Friedel-Crafts酰基化反应制得乙酰基二茂铁,接着通过Willgerodt-Kindler反应制得二茂铁乙酸,再经过还原反应得到了目标化合物2-二茂铁基乙醇。并在二茂铁乙酸还原成2-二茂铁基乙醇的反应中,探讨了不同反应条件对产物收率的影响。确定了最佳还原条件为:还原剂为氢化铝锂、物料比n (氢化铝锂):n (二茂铁乙酸)为8 : 1,溶剂为四氢呋喃,反应温度为25 C,反应时间为24 h,2-二茂铁基乙醇的收率为82 %。随后,初步的活性测试结果表明,2-二茂铁基乙醇对人乳腺癌细胞MCF-7和MDA-MB-231、人肝癌细胞HepG2、人宫颈癌细胞HeLa均有明显地抑制活性,其半数抑制浓度(IC50)值分别为17.4、12.9、20.7、24.6 μmol/L;此外,2-二茂铁基乙醇对正常的MCF-10A细胞没有毒性,而阳性对照药物5-FU展现出了一定的毒性。 相似文献
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分别将橙花醇和香叶醇(Ⅰ)(柠檬醛两个立体异构体的前体)氧化为相应的醛(Ⅱ),进一步氧化为酸(Ⅲ),然后与溴丙炔发生亲核取代反应得到末端炔酯(Ⅳ),最后与系列取代叠氮化合物发生Husigen环加成反应,得到26个(Z)-、(E)-柠檬醛基1,2,3-三唑类化合物(Ⅴa~m).采用FTIR、1HNMR、13CNMR和ESI-MS对目标化合物结构进行了表征,并测试了目标化合物的抑菌活性.结果表明:在目标化合物质量浓度为50 mg/L时,对西瓜炭疽病菌、黄瓜枯萎病菌、花生褐斑病菌、苹果轮纹病菌、小麦赤霉病菌、番茄早疫病菌、玉米小斑病菌和水稻纹枯病菌8种植物病原菌均显示出一定的抑菌活性,其中,(E)-柠檬醛基对-溴苄基1,2,3-三唑〔(E)-Ⅴm〕、(E)-柠檬醛基邻-甲基苄基1,2,3-三唑〔(E)-Ⅴb〕和(Z)-柠檬醛基间-甲基苄基1,2,3-三唑〔(Z)-Ⅴc〕对西瓜炭疽病菌的相对抑制率分别为95.2%(A级活性水平,优于阳性对照百菌清)、81.0%(B级活性水平)和81.0%(B级活性水平).此外,目标化合物(E)-Ⅴm对玉米小斑病菌的抑制率高达95.2%(A级活性水平,优于阳性对照百菌清).因此,化合物(E)-Ⅴm有望成为新的候选抑菌剂. 相似文献
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Guo-Xiang Sun Ming-Yan Yang Yan-Xia Shi Zhao-Hui Sun Xing-Hai Liu Hong-Ke Wu Bao-Ju Li Yong-Gang Zhang 《International journal of molecular sciences》2014,15(5):8075-8090
In order to investigate the biological activity of novel 1,2,4-triazole compounds, seventeen novel 1,2,4-triazole derivatives containing pyridine moiety were synthesized under microwave assistant condition by multi-step reactions. The structures were characterized by 1H NMR, MS and elemental analyses. The target compounds were evaluated for their fungicidal activities against Stemphylium lycopersici (Enjoji) Yamamoto, Fusarium oxysporum. sp. cucumebrium, and Botrytis cinerea in vivo, and the results indicated that some of the title compounds displayed excellent fungicidal activities. Theoretical calculation of the title compound was carried out with B3LYP/6-31G (d,p). The full geometry optimization was carried out using 6-31G (d,p) basis set, and the frontier orbital energy, atomic net charges were discussed, and the structure-activity relationship was also studied. 相似文献
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Dan Liu Ling Luo Zhengxing Wang Xiaoyun Ma Xiuhai Gan 《International journal of molecular sciences》2022,23(3)
Plant diseases that are caused by fungi and nematodes have become increasingly serious in recent years. However, there are few pesticide chemicals that can be used for the joint control of fungi and nematodes on the market. To solve this problem, a series of novel 1,2,4-oxadiazole derivatives containing amide fragments were designed and synthesized. Additionally, the bioassays revealed that the compound F15 demonstrated excellent antifungal activity against Sclerotinia sclerotiorum (S. sclerotiorum) in vitro, and the EC50 value of that was 2.9 μg/mL, which is comparable with commonly used fungicides thifluzamide and fluopyram. Meanwhile, F15 demonstrated excellent curative and protective activity against S. sclerotiorum-infected cole in vivo. The scanning electron microscopy results showed that the hyphae of S. sclerotiorum treated with F15 became abnormally collapsed and shriveled, thereby inhibiting the growth of the hyphae. Furthermore, F15 exhibited favorable inhibition against the succinate dehydrogenase (SDH) of the S. sclerotiorum (IC50 = 12.5 μg/mL), and the combination mode and binding ability between compound F15 and SDH were confirmed by molecular docking. In addition, compound F11 showed excellent nematicidal activity against Meloidogyne incognita at 200 μg/mL, the corrected mortality rate was 93.2%, which is higher than that of tioxazafen. 相似文献
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以2,4-二氯苯甲酸为起始原料,经酯化、肼解、成盐、闭环合成3-硫酮-4-氨基-5-(2,4-二氯)苯基-1,2,4-三唑(Ⅳ),然后与取代甲醛缩合生成中间体(Ⅴ),最后以乙腈为溶剂,K2CO3为催化剂,中间体Ⅴ与卤代烃于75℃反应2 h合成了8个含三唑Schiff碱硫醚衍生物(Ⅵa~Ⅵh),收率69%~78%,其结构经1HNMR、13CNMR、19FNMR、IR以及元素分析表征。初步生物活性测试结果表明,部分目标化合物对黄瓜霜霉病的抑制率达100%。 相似文献